Hoechst Aktiengesellschaft

Sanofi-a Ventis Deutschland Gmbh

Aventis Pharma Deutschland, Gmbh

Sanofi

Sanofi-aventis

Clariant Corporation

Hoechst Marion Roussel Deutschland Gmbh

Hoeschst Aktiengesellschaft

Heinz-Werner Kleemann

Andreas Gerhard Weichert

Jan-Robert Schwark

Udo Albus

Wolfgang Scholz

Hans-Jochen Lang

Joachim Brendel

Hans Jochen Lang

Hans-Willi Jansen

Stefan Peukert

Adalbert Wagner

Serge Mignani

Jean-Christophe Carry

Horst Hemmerle

Holger Heitsch

Baptiste Ronan

Gerrit Schubert

Sabine Faber

Bernward Scholkens

Heinrich Christian Englert

Armin Hofmeister

Stefan Petry

Arielle Genevois-Borella

Pascal Desmazeau

Wolfgang Linz

Hermann J Gerhards

Remo Weck

Gerhard Zoller

Hartmut Strobel

David William Will

Josef Pernerstorfer

Eugen Falk

Oliver Plettenburg

Paulus Wohlfart

Katrin Lorenz

Jean Bouquerel

Antony Bigot

Marcel Patek

Matthias Schaefer

Peter Crause

Alena Safarova

John Weston

Matthias Loehn

Joerg Rieke-Zapp

Gabriele Wiemer

Bao-Guo Huang

Reda Hanna

Carsten Struebing

Johannes Keil

Xiao-Dong Wu

Yves Gouraud

Hans-Jerg Kleiner

Gary A Flynn

Martin Bickel

Hansjorg Urbach

Rainer Henning

Klaus Wirth

Uwe Heinelt

Bansi Lal

Uwe Gerlach

Reinhard Becker

Michel Evers

Marc Nazare

Dieter Regnat

Olivier Duclos

Jean-Paul Vevert

Gilles Doerflinger

Sergio Mallart

Bernd Jablonka

Nis Halland

Jean-Michel Altenburger

Dirk Gretzke

Peter Below

Manfred Gerken

Jean-Paul Martin

Dieter Ruppert

Thomas M Boehme

Tilo Weiss

Stefania Pfeiffer-Marek

Hans-Ludwig Sch&auml;fer

Friedemann Schmidt

Bernhard Seuring

Alain Le Brun

Hartmut R&uuml;tten

Barbara Ann Anderson

Marc Nazaré

Bernard Pirard

Joachim Saas

Werner Seiz

Henning Vollert

Frederic Jeannot

Jean Bououerel

Thomas Böhme

Susanne Miehe

Thomas Bohme

John-Claude Caille

Frédéric Jeannot

The present invention relates to N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides of the formula I, wherein Ar, n, X, Z, R1, R2 and R3 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals

The present invention relates to compounds of the formula I, wherein A, Y, Z, Rto Rand Rhave the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPAreceptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Acylamino-substituted cyclic carboxylic acid derivatives and their use as pharmaceuticals

The present invention relates to compounds of the formula I, wherein A, Y, Z, Rto Rand Rhave the meanings indicated in the claims, which are pharmaceutically active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPAreceptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

The invention relates to substituted isoquinoline and isoquinolinones of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds. 

Substituted isoquinolines and isoquinolinones as Rho kinase inhibitors

TRPC ion channels are non-selective channels widely expressed in human tissues. These channels are involved in numerous physiological functions and are putative targets for the development of novel medicines. There is a need to gain a better understanding of TRPC ion channels in cells and beyond. The present invention provides a pharmacological tool compound that allows to study TRPC ion channels due to its discriminating inhibition of TRPC subfamilies. In the present invention, norgestimate is shown to selectively inhibit TRPC3, TRPC6 and TRPC7.

Use of norgestimate as a selective inhibitor of TRPC3, TRPC6 and TRPC7 ion channels

Pentafluorosulfanylbenzoylguanidines of the formula I and II in which R1 to R4 have the meanings stated in the claims, are suitable as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris. They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.

Pentafluorosulfanylbenzoylguanidines, processes for their preparation, their use as medicaments or diagnostic aids, and medicaments comprising them

The invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds. 

6-substituted isoquinolines and isoquinolinones

The present invention relates to heteroarylacrylamides of the formula I, in which Het, X, R, R, R, Rand Rhave the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Heteroarylacrylamides and their use as pharmaceuticals

The present invention relates to processes for preparing (3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetylguanidine derivatives of the formula I via 3-hydroxy-2,3-dihydro-1H-isoindol-1-one derivatives or 3-(2-carbamoylphenyl)-acrylic ester derivatives as intermediates, to a process for optical resolution, and to intermediates of the process according to the invention.

Process for preparing (3-oxo-2,3-dihydro-1H-isoindol-1-yl) acetylguanidine derivatives

The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R, Rand Rhave the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Heteroaryl-substituted carboxamides and their use as pharmaceuticals

The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar, Ar, Rand Rhave the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Di(hetero)arylcyclohexane derivatives, their preparation, their use and pharmaceutical compositions comprising them

Pentafluorosulfanylbenzoylguanidines, of the formula I and II in which R1 to R4 have the meanings stated in the claims, are suitable as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris. They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.

Pentafluorosulfanyl-benzenes according to Formula (I): a process for their preparation and their use as valuable synthetic intermediates for preparing, for example, medicaments, diagnostic aids, liquid crystals, polymers, pesticides, herbicides, fungicides, nematicides, parasiticides, insecticides, acaricides and arthropodicides.

Ortho-substituted pentafluorosulfanylbenzenes, process for their preparation and their use as valuable synthetic intermediates

The present invention relates to substituted benzoylguanidines of the formula I: in which R1 to R8 and X and Y are as described in the specification, and their pharmaceutically acceptable salts are substituted acylguanidines as inhibitors of the cellular sodium-proton antiporter (Na/Hexchanger, NHE).

Substituted benzoylguanidines, method for production and use thereof as medicament or diagnostic and medicament comprising the same

This invention relates to novel substituted pentafluorosulfanylbenzenes of the formula I: and/or salts thereof as claimed, for use as a synthetic intermediates for preparing medicaments, diagnostic aids, liquid crystals, pesticides, herbicides, fungicides, nematicides, parasiticides, insecticides, acaricides, arthropodicides and polymers.

Ortho-substituted pentafluorosulfanyl benzenes, method for the production thereof and their use as synthesis intermediates

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Bischofsheim, Germany

Heinz-Werner Kleemann